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目的合成并表征了一个新的奥沙利铂类似物,顺式-叶酸根.(1R,2R-环己二胺)合铂(II)([Pt(DACH)FA]),以期获得抗癌活性优于奥沙利铂的新铂配合物。方法采用MTT法,评价了[Pt(DACH)FA]对A549,BGC-823,HCT-116和COLO320人癌细胞株的体外抗癌活性。结果[Pt(DACH)FA]在HCT-116和COLO320细胞株中有活性,IC50值分别为50.1μmol.L-1和25.0μmol.L-1,而在A549和BGC-823细胞株中则活性很低。结论虽然[Pt(DACH)FA]在HCT-116和COLO320细胞株中有一定的抗癌活性,但是在所评价的细胞株中活性均小于阳性对照药奥沙利铂,说明用叶酸根作为解离基团降低了该铂配合物的细胞毒性。
OBJECTIVE To synthesize and characterize a new oxaliplatin analog, cis-folate (1R, 2R-cyclohexanediamine) platinum (II) ([Pt (DACH) FA] Activity is better than oxaliplatin new platinum complexes. Methods MTT assay was used to evaluate the antitumor activity of [Pt (DACH) FA] in A549, BGC-823, HCT-116 and COLO320 human cancer cell lines in vitro. Results [Pt (DACH) FA] was active in HCT-116 and COLO320 cell lines with IC50 values of 50.1 μmol.L-1 and 25.0 μmol·L-1, respectively, whereas the activity in A549 and BGC-823 cell lines Very low. Conclusions Although [Pt (DACH) FA] has some anticancer activity in HCT-116 and COLO320 cell lines, its activity in the cell lines evaluated is less than that of the positive control oxaliplatin, indicating that the use of folate as a solution The leaving group reduces the cytotoxicity of the platinum complex.